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A 205804

Catalog No.GC15557

E-selectin/ICAM-1 expression inhibitor

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A 205804 Chemical Structure

Cas No.: 251992-66-2

Size Price Stock Qty
10mg
$57.00
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50mg
$245.00
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500mg
$618.00
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1g
$927.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

A-205804 is a potent and selective inhibitor of E-selectin and ICAM-1 with IC50 value of 20 nM and 25 nM, respectively [1].

E-selectin is a cell adhesion molecule and plays an important role in recruiting leukocytes to injury site during inflammation process. ICAM-1 (intracellular adhesion molecule 1) is a ligand for LFA-1 and involves in leukocytes binding to endothelial cells process. It has been reported that abnormal expression of E-selectin and ICAM-1 are correlated with a variety of cancers [2].

A-205804 is a selective E-selectin and ICAM-1 inhibitor over VCAM-1. When tested with primary HUVECs cells, A-205804 treatment reduced cell migration ability by inhibiting the expression of E-selectin and ICAM-1 [3]. In human vascular endothelial cells using whole-cell high-throughput assay, it was shown that A-205804 exhibited potent and selective inhibition to E-selectin and ICAM-1 with low concentrations [1]. Further, it was revealed that A-205804 inhibited E-selectin and ICAM-1 expressions by translocating to cell nucleus and noncovalently associated with macromolecules of molecular weight greater than 650 kDa when tested with human umbilical vein endothelial cells (HUVECs) [4].

References:
[1].  Stewart, A.O., et al., Discovery of inhibitors of cell adhesion molecule expression in human endothelial cells. 1. Selective inhibition of ICAM-1 and E-selectin expression. J Med Chem, 2001. 44(6): p. 988-1002.
[2].  Chang, C.Z., et al., Valproic acid attenuates intercellular adhesion molecule-1 and E-selectin through a chemokine ligand 5 dependent mechanism and subarachnoid hemorrhage induced vasospasm in a rat model. J Inflamm (Lond), 2015. 12: p. 27.
[3].  Zhu, G.D., et al., Selective inhibition of ICAM-1 and E-selectin expression in human endothelial cells. 2. Aryl modifications of 4-(aryloxy)thieno[2,3-c]pyridines with fine-tuning at C-2 carbamides. J Med Chem, 2001. 44(21): p. 3469-87.
[4].   Zhu, G.D., et al., Synthesis and mode of action of (125)I- and (3)H-labeled thieno[2,3-c]pyridine antagonists of cell adhesion molecule expression. J Org Chem, 2002. 67(3): p. 943-8.

Chemical Properties

Cas No. 251992-66-2 SDF
Chemical Name 4-(4-methylphenyl)sulfanylthieno[2,3-c]pyridine-2-carboxamide
Canonical SMILES CC1=CC=C(C=C1)SC2=C3C=C(SC3=CN=C2)C(=O)N
Formula C15H12N2OS2 M.Wt 300.39
Solubility ≥ 30mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.329 mL 16.645 mL 33.2901 mL
5 mM 0.6658 mL 3.329 mL 6.658 mL
10 mM 0.3329 mL 1.6645 mL 3.329 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 24 reference(s) in Google Scholar.)

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